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EP2042490A3 - Benzimidazole derivatives as vanilloid receptor antagonists - Google Patents

Benzimidazole derivatives as vanilloid receptor antagonists Download PDF

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Publication number
EP2042490A3
EP2042490A3 EP08171574A EP08171574A EP2042490A3 EP 2042490 A3 EP2042490 A3 EP 2042490A3 EP 08171574 A EP08171574 A EP 08171574A EP 08171574 A EP08171574 A EP 08171574A EP 2042490 A3 EP2042490 A3 EP 2042490A3
Authority
EP
European Patent Office
Prior art keywords
receptor antagonists
benzimidazole derivatives
vanilloid receptor
compounds
formula
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP08171574A
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German (de)
French (fr)
Other versions
EP2042490A2 (en
Inventor
Yevgeni Besidski
Inger Kers
Martin Nylöf
Andis Slaitas
Mats Svensson
Didier Rotticci
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AstraZeneca AB
Original Assignee
AstraZeneca AB
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Publication date
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Publication of EP2042490A2 publication Critical patent/EP2042490A2/en
Publication of EP2042490A3 publication Critical patent/EP2042490A3/en
Withdrawn legal-status Critical Current

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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/16Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic the nitrogen atom of the amino group being further bound to carbon atoms of six-membered aromatic rings
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    • C07C229/54Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C229/56Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in ortho-position
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/12Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • C07C233/15Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
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    • C07C233/00Carboxylic acid amides
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    • C07C233/45Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/46Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/47Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
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    • C07C317/32Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/36Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atoms of the amino groups bound to hydrogen atoms or to carbon atoms
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    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Pulmonology (AREA)
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  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
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Abstract

The present invention relates to new compounds of formula I,
Figure imga0001
wherein R1 to R9 are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
EP08171574A 2003-05-16 2004-05-13 Benzimidazole derivatives as vanilloid receptor antagonists Withdrawn EP2042490A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SE0301446A SE0301446D0 (en) 2003-05-16 2003-05-16 New Compounds
SE0400043A SE0400043D0 (en) 2003-05-16 2004-01-12 New compounds
EP04732865A EP1626964B1 (en) 2003-05-16 2004-05-13 New benzimidazole derivatives

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
EP04732865A Division EP1626964B1 (en) 2003-05-16 2004-05-13 New benzimidazole derivatives

Publications (2)

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EP2042490A2 EP2042490A2 (en) 2009-04-01
EP2042490A3 true EP2042490A3 (en) 2009-09-30

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EP04732865A Expired - Lifetime EP1626964B1 (en) 2003-05-16 2004-05-13 New benzimidazole derivatives
EP08171574A Withdrawn EP2042490A3 (en) 2003-05-16 2004-05-13 Benzimidazole derivatives as vanilloid receptor antagonists

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US (1) US7645784B2 (en)
EP (2) EP1626964B1 (en)
JP (1) JP4762903B2 (en)
KR (1) KR101110404B1 (en)
CN (2) CN101328150A (en)
AR (1) AR044342A1 (en)
AT (1) ATE421506T1 (en)
AU (2) AU2004238177B2 (en)
BR (1) BRPI0410316A (en)
CA (1) CA2525628C (en)
CO (1) CO5631436A2 (en)
CY (1) CY1108894T1 (en)
DE (1) DE602004019208D1 (en)
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ES (1) ES2319529T3 (en)
HK (1) HK1085735A1 (en)
HR (1) HRP20090167T1 (en)
IL (1) IL199668A0 (en)
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MX (1) MXPA05012247A (en)
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NZ (1) NZ543075A (en)
PL (1) PL1626964T3 (en)
PT (1) PT1626964E (en)
RU (1) RU2337098C2 (en)
SE (2) SE0301446D0 (en)
SG (2) SG171471A1 (en)
SI (1) SI1626964T1 (en)
TW (1) TWI333950B (en)
UA (1) UA85842C2 (en)
WO (1) WO2004100865A2 (en)
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WO2022211518A1 (en) * 2021-04-02 2022-10-06 파렌키마바이오텍 주식회사 Novel compound and use thereof in treating psoriasis, asthma, or systemic lupus erythematosus
DE102022104759A1 (en) 2022-02-28 2023-08-31 SCi Kontor GmbH Co-crystal screening method, in particular for the production of co-crystals

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